title: Syntheses of 1,2,3-triazolyl salicylamides with inhibitory activity on lipopolysaccharide-induced nitric oxide production.
abstract: A 28-membered 1,2,3-triazolyl salicylamide library was synthesized via a Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition and evaluated for their abilities to inhibit NO production in LPS-activated RAW264.7 macrophage cells. Among 28 analogues, 29 g showed a significant inhibitory activity (IC(50) = 12.8 μM). The inhibitory effects of 29 g on LPS-mediated NO production in macrophage cells appeared to be associated with the suppression of iNOS expression.
authors.affiliation: Division of Life and Pharmaceutical Sciences, Ewha Womans University, Center for Cell Signaling and Drug Discovery Research, College of Pharmacy, 11-1 Daehyun-Dong, Seodaemun-Gu, Seoul 120-750, Republic of Korea.
authors.forename: Jieun
authors.initials: J
authors.lastname: Yoon
authors.forename: Lan
authors.initials: L
authors.lastname: Cho
authors.forename: Sang Kook
authors.initials: SK
authors.lastname: Lee
authors.forename: Jae-Sang
authors.initials: JS
authors.lastname: Ryu
mesh_terms: D000818:Animals; D002460:Cell Line; D020128:Inhibitory Concentration 50; D008070:Lipopolysaccharides / Q000494:pharmacology*; D051379:Mice; D009569:Nitric Oxide / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D052247:Nitric Oxide Synthase Type II / Q000037:antagonists & inhibitors / Q000378:metabolism; D012457:Salicylamides / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D008070:Lipopolysaccharides; D012457:Salicylamides; D009569:Nitric Oxide; D052247:Nitric Oxide Synthase Type II